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NCI

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175

Inhibitors & Agonists

2

Fluorescent Dye

1

Biochemical Assay Reagents

1

Peptides

3

Inhibitory Antibodies

29

Natural
Products

4

Click Chemistry

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148517
    AZD0095
    4 Publications Verification

    Monocarboxylate Transporter Cancer
    AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205) .
    AZD0095
  • HY-132295
    Azenosertib
    4 Publications Verification

    ZN-c3

    Wee1 Cancer
    Azenosertib (ZN-c3) is a selective, orally active inhibitor for Wee1 inhibitor (IC50=3.9 nM). Azenosertib exhibits antitumor activity .
    Azenosertib
  • HY-101130
    PNU-74654
    Maximum Cited Publications
    11 Publications Verification

    Wnt β-catenin Apoptosis Cancer
    PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
    PNU-74654
  • HY-101567
    BMS-986158
    3 Publications Verification

    Epigenetic Reader Domain Cancer
    BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively .
    BMS-986158
  • HY-N0840
    Bruceantin
    2 Publications Verification

    (-)-Bruceantin; NCI165563; NSC165563

    c-Myc Caspase Mitochondrial Metabolism Apoptosis Parasite Infection Cancer
    Bruceantin ((-)-Bruceantin) is a quassinoid found in B. javanica. Bruceantin activates caspase signaling pathway, causes the mitochondrial dysfunction, inhibits cell proliferation, induces cell differentiation and apoptosis. Bruceantin exhibits anti-leukemia and antiprotozoal activities .
    Bruceantin
  • HY-147858

    PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC EGFR degrader 7
  • HY-D1161

    NCI 240899

    Fluorescent Dye Neurological Disease
    True Blue (NCI 240899) is a fluorescent dye, as neuronal retrograde tracer (excitation wavelength 395-425 nm, barrier filter 450 nm). True Blue can label neuron and has no effects on neuronal survival .
    True Blue
  • HY-149265

    Reactive Oxygen Species (ROS) TrxR Ferroptosis Apoptosis Cancer
    ROS-generating agent 1 (Compound 2c) covalently modifies the Sec-498 residue of TrxR to generate ROS. ROS-generating agent 1 reduces intracellular TrxR protein level. ROS-generating agent 1 results in ROS-dependent apoptosis and ferroptosis of NCI-H460 cells. ROS-generating agent 1 has anti-cancer activities .
    ROS-generating agent 1
  • HY-176798

    Lactate Dehydrogenase Reactive Oxygen Species (ROS) Apoptosis Cancer
    NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targets glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model .
    NCI-006
  • HY-176557

    Deubiquitinase Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase Autophagy Cancer
    NCI677397 is a USP24 inhibitor. NCI677397 increases lipid ROS, activates cholesterol and fatty acid biosynthesis, degrades ABC transporters, GPX4 and DHFR through the autophagy pathway, decreases the level of P-gp and ultimately leads to ferroptosis in drug-resistant cancer cells. NCI677397 can be used for the study of lung caner and brain cancer .
    NCI677397
  • HY-N2039

    Others Cancer
    20(R)-Ginsenoside Rg2 shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities .
    20(R)-Ginsenoside Rg2
  • HY-100555

    HSP Infection Cancer
    CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
    CH5138303
  • HY-147208

    YAP Cancer
    MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
    MSC-4106
  • HY-156215

    HCV Infection
    NCI-B16 is a small molecule RNA binder and inhibits HCV viral replication .
    NCI-B16
  • HY-19797

    p97 Cancer
    ML241 is a potent, selective and competitive p97 ATPase inhibitor with an IC50 of 0.11 μM. ML241 can be used for the research of cancer .
    ML241
  • HY-116505

    JAK Cancer
    JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM) .
    JAK1-IN-4
  • HY-W779529

    2'-Acetylneriifolin

    Na+/K+ ATPase Cancer
    Cerberin is a cardiac glycoside that has been found in C. odollam and has cytotoxic and cardiac modulatory activities. It is cytotoxic to KB and NCI H187 cancer cells (IC50s=1.92 and 1.24 μg/mL).1 Cerberin inhibits Na+/K+-ATPase, increasing intracellular sodium levels and action potential duration in cardiac cells.
    Cerberin
  • HY-164384

    PI3K Akt mTOR Apoptosis Cancer
    DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
    DFX117
  • HY-156060

    Toll-like Receptor (TLR) Inflammation/Immunology
    NCI126224 is a TLR4 signaling inhibitor. NCI126224 suppress LPS (HY-D1056)-induced production of NF-κB, TNF-α, IL-1β, and NO in the nanomolar-low micromolar range. NCI126224 can be used for the research of inflammatory diseases .
    NCI126224
  • HY-U00095
    Hepsulfam
    2 Publications Verification

    NCI 329680; ZINC01574758

    DNA Alkylator/Crosslinker Cancer
    Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.
    Hepsulfam
  • HY-171958

    PROTACs EGFR Cancer
    PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFR L858R-T790M (NCI-H1975 cells), EGFR L858R (NCI-H3255 cells), and EGFR L858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM .
    PROTAC EGFR degrader 12
  • HY-W1117786

    ADC Payload NAMPT Cancer
    Nampt-IN-10 (Compound 4) is an efficient inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). Nampt-IN-10 exhibits nanomolar-level inhibitory activity against cell lines such as MDA-MB453, NCI-N87, and NCI-H526. Nampt-IN-10 can be used as an ADC payload, and the ADC constructed with it as the core demonstrates significant anti-tumor activity .
    Nampt-IN-10
  • HY-178242

    PROTACs EGFR Cancer
    PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand (HY-178313); Blue: CRBN ligand (HY-W1128702); Black: Linker; EGFR ligand + Linker (HY-178311)) .
    PROTAC EGFR degrader 16
  • HY-179403

    Ras Cancer
    KRASG12C IN-17 is an orally active covalent KRAS G12C inhibitor, showing strong inhibitory activity in KRAS G12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRAS G12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer .
    KRASG12C IN-17
  • HY-157673

    16:1 PE

    Phosphatase Apoptosis Cancer
    1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance PP2A and PTP1B activities in malignant pleural mesothelioma cells. 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis of NCI-H28 malignant pleural mesothelioma cells .
    1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine
  • HY-U00095R

    NCI 329680 (Standard); ZINC01574758 (Standard)

    DNA Alkylator/Crosslinker Reference Standards Cancer
    Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.
    Hepsulfam (Standard)
  • HY-U00155

    NSC172112; NSC268497

    DNA Alkylator/Crosslinker Cancer
    NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
    NCI172112
  • HY-160129

    ML-970; AS-I-145; NSC 716970

    Nucleoside Antimetabolite/Analog Cancer
    Centanamycin (ML-970; AS-I-145; NSC 716970) is a novel DNA-binding agent, and shows cytotoxic activity, with an average GI50 of 34 nM in NCI-60 cell line screening .
    Centanamycin
  • HY-172426

    Anaplastic lymphoma kinase (ALK) Cancer
    Dirozalkib (Compound 4) is the inhibitor for ALK with an IC50 of 0.9 nM. Dirozalkib exhibits anti-proliferative activity in cancer cells NCI-H3122, Karpas-299 and NCI-H2228 with IC50s of 130.4, 0.71 and 15.11 nM, respectively. Dirozalkib exhibits good pharmacokinetics characteristics with an bioavailbility of 30%~50% .
    Dirozalkib
  • HY-W056098

    PROTAC Linkers Cancer
    tert-Butyl N-[cis-3-(aminomethyl)cyclobutyl]carbamate is a PROTAC linker that can be used in the synthesis of PROTACs.
    tert-Butyl N-[cis-3-(aminomethyl)cyclobutyl]carbamate
  • HY-170764

    YAP Cancer
    M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC50 value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC50 value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model .
    M3686
  • HY-147703

    Aurora Kinase Cancer
    Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
    Aurora kinase inhibitor-9
  • HY-173259

    PARP Cancer
    PARP7-IN-23 (compound 56) is a potent PARP7 inhibitor with an EC50 of 0.915 nM for pSTAT1 in NCI-H1373 cells. PARP7-IN-23 has the potential for cancer research .
    PARP7-IN-23
  • HY-173262

    PARP Cancer
    PARP7-IN-24 (compound 44) is a potent PARP7 inhibitor with an EC50 of 0.375 nM for pSTAT1 in NCI-H1373 cells. PARP7-IN-24 has the potential for cancer research .
    PARP7-IN-24
  • HY-178941

    Dihydroorotate Dehydrogenase Apoptosis Caspase Reactive Oxygen Species (ROS) Cancer
    DHODH-IN-32 (Compound A1) is a DHODH inhibitor. DHODH-IN-32 shows significant cytotoxicity against NCI-60 cell lines, especially being sensitive to breast cancer, prostate cancer and leukemia cell lines. DHODH-IN-32 can induce cell apoptosis by activating the Caspase pathway. DHODH-IN-32 causes G0/G1 phase cell cycle arrest and inhibits cellular metabolism by ROS. DHODH-IN-32 exhibits significant anti-tumor properties in mouse breast cancer models. DHODH-IN-32 can be used for the study of breast cancer .
    DHODH-IN-32
  • HY-157085

    HSP Cancer
    BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice .
    BX-2819
  • HY-170912

    Topoisomerase Apoptosis ROS Kinase Cytochrome P450 Caspase Bcl-2 Family PI3K Akt mTOR Cancer
    Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .
    Topo I/II-IN-2
  • HY-176538

    HSP Cancer
    Antiproliferative agent-72 (Compound 10) is a Hsp90 inhibitor with a Kd of 11 nM. Antiproliferative agent-72 has antiproliferative activity with IC50s of 1.5  μM and 1.1 μM for HCT116 and NCI-N87 cells, respectively. Antiproliferative agent-72 can be used for cancers research .
    Antiproliferative agent-72
  • HY-157522

    Phosphodiesterase (PDE) Cancer
    NCI-14465 is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP1) inhibitor with an IC 50 of 26.4 μM. NCI-14465 can be used in cancer research .
    NCI-14465
  • HY-U00155R

    NSC172112 (Standard); NSC268497 (Standard)

    Reference Standards DNA Alkylator/Crosslinker Cancer
    NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
    NCI172112 (Standard)
  • HY-163000

    EGFR Cancer
    EGFR-IN-129 (Compound 10b) is a potent and selective EGFR inhibitor, with an IC50 of 51.2 nM. EGFR-IN-129 exhibits broadest-spectrum antiproliferative activity against the NCI-tumor panel .
    EGFR-IN-129
  • HY-N14255

    Antibiotic Bacterial Infection Cancer
    Memnobotrin A is an antibiotic found in Memnoniella echinata (JS6308). Memnobotrin A has inhibitory effect on NCI-460, MCF7 and SF-268 cell lines .
    Memnobotrin A
  • HY-123597

    DDUG; NCI C04808

    Autophagy Checkpoint Kinase (Chk) Cancer
    NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
    NSC 109555
  • HY-N14280

    Antibiotic Bacterial Infection Cancer
    Memnobotrin B is an antibiotic found in Memnoniella echinata (JS6308). Memnobotrin B has inhibitory effect on NCI-460, MCF7 and SF-268 cell lines .
    Memnobotrin B
  • HY-125730

    Others Cancer
    Kibdelone A is a type of natural compound from the flavonoid family, and it has potential value as an anti-proliferative agent .
    Kibdelone A
  • HY-N3443

    Others Cancer
    Jolkinol A is a natural product that can be found in Euphorbia pubescens. Jolkinol A inhibits cell growth with GI50s of 95.3, 57.3, >100 µM for MCF-7, NCI-460, SF-268 cells, respectively .
    Jolkinol A
  • HY-147724

    Microtubule/Tubulin Cancer
    Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
    Microtubule inhibitor 3
  • HY-147728

    Microtubule/Tubulin Cancer
    Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
    Microtubule inhibitor 7
  • HY-168093

    Ferroptosis Cancer
    Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
    Cetzole
  • HY-N10307

    Fungal Bacterial Endogenous Metabolite Infection Cancer
    Anserinone B is an antifungal and antibacterial benzoquinone. Anserinone B causes radial growth reductions of 50% and 37% against S.fimicola and A. furfuraceus, respectively. Anserinones B also displays moderate cytotoxicity in the NCI’s 60 human tumor cell line panel (GI50=4.4 µg/mL) .
    Anserinone B

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